Biological Activity
Inhibitor of checkpoint kinase 1 (Chk1) that displays selectivity over other protein kinases (IC50 values are 15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively). Abrogates G2 cell cycle arrest caused by γ-irradiation and topoisomerase I inhibition. Potentiates cytotoxicity of DNA-damaging drugs, enhancing the efficacy of some chemotherapeutics.
Compound Libraries
SB 218078 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 393.39 |
| Formula | C24H15N3O3 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 135897-06-2 |
| PubChem ID | 3387354 |
| InChI Key | OTPNDVKVEAIXTI-UHFFFAOYSA-N |
| Smiles | O=C1NC(=O)C2=C1C1=C3N(C4CCC(O4)N4C5=C(C=CC=C5)C2=C34)C2=CC=CC=C12 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.34 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 393.39. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.54 mL | 12.71 mL | 25.42 mL |
| 5 mM | 0.51 mL | 2.54 mL | 5.08 mL |
| 10 mM | 0.25 mL | 1.27 mL | 2.54 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Jackson et al (2000) An indolocarbazole inhibitor of human checkpoint kinase (Chk1) abrogates cell cycle arrest caused by DNA damage. Cancer Res. 60 566 PMID: 10676638
Kawabe (2004) G2 checkpoint abrogators as anticancer drugs. Mol.Cancer Ther. 3 513 PMID: 15078995
Chen et al (2006) Checkpoint kinase 1-mediated phosphorylation of cdc25C and bad proteins are involved in antitumor effects of loratadine-induced G2/M phase cell-cycle arrest and apoptosis. Mol.Carcinogenesis 45 461 PMID:
Keywords: SB 218078, supplier, inhibitors, inhibits, checkpoint, kinase, 1, Chk1, Chk2, Checkpoint, Kinases, Control, SB218078, Checkpoint, Kinases, Checkpoint, Control, Kinases, Checkpoint, Kinases, Tocris Bioscience
